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A7063858

Bimiralisib(PQR309) , 10mMinDMSO , 1225037-39-7

CAS NO.:1225037-39-7

Empirical Formula: C17H20F3N7O2

Molecular Weight: 411.38

MDL number:

Pack Size Price Stock Quantity
1ml RMB559.20 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Boiling point: 643.7±65.0 °C(Predicted)
Density  1.418±0.06 g/cm3(Predicted)
storage temp.  Store at -20°C
solubility  DMSO:22.0(Max Conc. mg/mL);53.48(Max Conc. mM)
DMF:10.0(Max Conc. mg/mL);24.31(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);4.86(Max Conc. mM)
form  A crystalline solid
pka 4.92±0.10(Predicted)
color  White to gray

Description and Uses

Bimiralisib is a potent and orally bioavailable inhibitor of phosphatidylinositol 3-kinases (PI3Ks; IC50s = 33, 661, 708, and 451 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively) and the mammalian target of rapamycin (mTOR; IC50 = 89 nM). It is selective for these kinases over a panel of cell surface and nuclear receptors, membrane channels, transporters, kinases, proteases, and phosphodiesterases at a concentration of 10 μM. Bimiralisib has anticancer activity with an average GI50 value of 0.7 μM across the National Cancer Institute (NCI) 60 human cancer cell line panel. In vivo, bimiralisib (5-15 mg/kg) reduces tumor growth in a dose-dependent manner in a PC3 prostate cancer mouse xenograft model. Formulations containing bimiralisib are under clinical investigation for the treatment of relapsed and refractory lymphoma and advanced solid tumors.

Bimiralisib is an orally bioavailable PI3K/mTOR inhibitor for cancer

Safety

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